Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMTP1DC)

Drug Name

Irbesartan Drug Info

Synonyms

irbesartan; 138402-11-6; Aprovel; Avapro; Karvea; SR-47436; BMS-186295; BMS 186295; Irbesartan [USAN:INN]; SR 47436; UNII-J0E2756Z7N; CHEMBL1513; 8-butyl-7-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-7,9-diazaspiro[44]non-8-en-6-one; CHEBI:5959; C25H28N6O; YOSHYTLCDANDAN-UHFFFAOYSA-N; J0E2756Z7N; 2-butyl-3-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1,3-diazaspiro[44]non-1-en-4-one; 3-((2'-(1H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-1,3-diazaspiro[44]non-1-en-4-one; NCGC00095122-01; AK-57149; DSSTox_CID_3169; Aprovel; Irbesarran; Irbetan; Lrbesartan; BMS Brand of Irbesartan; Bristol Myers Brand of Irbesartan; SanofiWinthrop Brand of Irbesartan; Aprovel (TN); Avalide (TN); Avapro (TN); Karvea (TN); Irbesartan (JAN/USAN/INN); BMS-186295, SR-47436,Aprovel, Karvea, Irbesartan; 2-Butyl-3-(p-(o-1H-tetrazol-5-ylphenyl)benzyl)-1,3-diazaspiro(44)non-1-en-4-one; 2-Butyl-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]1,3-diaza-spiro[44]non-1-en-4-one; 2-butyl-3-[ p-(o-1 H-tetrazol-5-ylphenyl)benzyl]-1,3-diazaspiro[4,4]non-1-en-4-one; 2-butyl-3-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]-1,3-diazaspiro[44]non-1-en-4-one; 2-butyl-3-{[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl}-1,3-diazaspiro[44]non-1-en-4-one; 2-n-butyl-3-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1,3-diazaspiro(4,4)non-1-en-4-one; [3H]irbesartan

Indication

Disease Entry	ICD 11	Status	REF
Hypertension	BA00-BA04	Approved	[1] , [2]

Therapeutic Class

Antihypertensive Agents

Cross-matching ID

PubChem CID: 3749
ChEBI ID: CHEBI:5959
CAS Number: CAS 138402-11-6
TTD Drug ID: DMTP1DC
VARIDT Drug ID: DR00482
INTEDE Drug ID: DR0879
ACDINA Drug ID: D00330

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiotensin II receptor type-1 (AGTR1)	TT8DBY3	AGTR1_HUMAN	Antagonist	[3] , [4]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Peptide transporter 1 (SLC15A1)	DT9G7XN	S15A1_HUMAN	Approved	[5]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[6]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[7]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Approved	[8]
Prostaglandin G/H synthase 1 (COX-1)	DE073H6	PGH1_HUMAN	Approved	[9]
UDP-glucuronosyltransferase 1A3 (UGT1A3)	DEF2WXN	UD13_HUMAN	Approved	[9]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Angiotensin II receptor type-1 (AGTR1)	DTT	AGTR1	9.315	6.241	6.761	5.625
Peptide transporter 1 (SLC15A1)	DTP	PEPT1	3.807	4.52	5.285	7.133
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089
Prostaglandin G/H synthase 1 (COX-1)	DME	PTGS1	6.09	7.747	6.04	7.023

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Hypertension

ICD Disease Classification

BA00-BA04

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Angiotensin II receptor type-1 (AGTR1)	DTT	AGTR1	8.95E-01	1.34E-02	0.07
Peptide transporter 1 (SLC15A1)	DTP	PEPT1	4.57E-01	2.15E-02	1.72E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	1.82E-04	-1.35E-01	-5.84E-01
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	1.90E-01	-9.81E-03	-5.96E-02
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.04E-02	6.29E-02	3.54E-01
Prostaglandin G/H synthase 1 (COX-1)	DME	PTGS1	3.97E-03	1.56E-01	4.33E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 589).
2	New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22.
3	Radioligand binding assays: application of [(125)I]angiotensin II receptor binding. Methods Mol Biol. 2009;552:131-41.
4	Binding characteristics of [(3)H]-irbesartan to human recombinant angiotensin type 1 receptors. J Renin Angiotensin Aldosterone Syst. 2000 Jun;1(2):159-65.
5	High-affinity interaction of sartans with H+/peptide transporters. Drug Metab Dispos. 2009 Jan;37(1):143-9.
6	Drug interactions with irbesartan. Clin Pharmacokinet. 2001;40(8):605-14.
7	Rapid detection of the known SNPs of CYP2C9 using oligonucleotide microarray. World J Gastroenterol. 2003 Jun;9(6):1342-6.
8	Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78.
9	Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.